CN118076334A - Oral composition - Google Patents

Oral composition Download PDF

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Publication number
CN118076334A
CN118076334A CN202280063104.XA CN202280063104A CN118076334A CN 118076334 A CN118076334 A CN 118076334A CN 202280063104 A CN202280063104 A CN 202280063104A CN 118076334 A CN118076334 A CN 118076334A
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China
Prior art keywords
fluorine
retention
salt
oral composition
oral
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CN202280063104.XA
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Chinese (zh)
Inventor
今崎麻里
小熊友一
岩崎彩佳
桥本匡太
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Lion Corp
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Lion Corp
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/20Halogens; Compounds thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/20Halogens; Compounds thereof
    • A61K8/21Fluorides; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/24Phosphorous; Compounds thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/55Phosphorus compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q11/00Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Chemical & Material Sciences (AREA)
  • Inorganic Chemistry (AREA)
  • Oral & Maxillofacial Surgery (AREA)
  • Cosmetics (AREA)

Abstract

The present application provides an oral composition containing a fluorine-containing compound, which has excellent fluorine ion retention on tooth surfaces and oral mucosa in the oral cavity and can impart excellent fluorine ion retention even after long-term storage. An oral composition comprising (A) condensed phosphoric acid or a salt thereof, (B) a calcium salt, (C) a fluorine-containing compound, and (D) pyrrolidone carboxylic acid or a salt thereof.

Description

Oral composition
Technical Field
The present invention relates to an oral composition which is excellent in fluoride ion retention on tooth surfaces and mucous membranes in the oral cavity and which can impart excellent fluoride ion retention even after long-term storage.
Background
Fluorine-containing compounds such as sodium fluoride are widely used in oral compositions such as dentifrice compositions as pharmaceutical ingredients having the functions of promoting recalcification, inhibiting decalcification, etc., for the purpose of preventing caries and the like. To make the fluorochemical function effectively, it is expected that: it is effective to retain the fluoride ion in the mucous membrane and tooth surface of the oral cavity for a long period of time, and even after the oral cavity is rinsed with water after use, a large amount of fluoride ion remains in the oral cavity.
As a method for improving the retention of fluoride ions, a method of allowing calcium ions to coexist with fluoride ions is used, but when calcium ions and fluoride ions coexist, calcium fluoride, which is an insoluble substance before acting on teeth, cannot exert a sufficient effect and the effect after storage is insufficient.
Patent document 1 (japanese patent application laid-open No. 10-511956) proposes a method of mixing these 2 compositions before applying calcium ions and fluorine ions to the oral cavity, but in this method, fluorine ions are immediately washed out by saliva because they enter the oral cavity, and a sufficient retention effect cannot be exhibited, and calcium fluoride is precipitated in a short time after mixing the 2 components, and thus fluorine ions cannot be sufficiently released, and an effect cannot be exhibited.
Patent document 2 (japanese patent application laid-open No. 2009-137863) proposes a composition in which a complex of a polyphosphate, a calcium salt, and a fluoride salt is prepared in advance, but this method has a problem that the retention of fluoride ions in the oral cavity is reduced after long-term storage, particularly in a dentifrice formulation.
Further, patent document 3 (international publication No. 2013/47826) proposes: an oral composition comprising a lactam compound having a lactam skeleton and an acidic group, such as pyrrolidone carboxylic acid or a salt thereof, and a fluorine compound, has an excellent dentin caries-suppressing effect. Patent document 4 (japanese patent application laid-open No. 2017-48162) proposes an oral composition containing a lactam compound and a water-insoluble calcium salt having a predetermined average particle diameter, which has an improved dentin caries inhibitory effect. However, these effects on dentin remain, and there is room for improvement in retention on mucous membranes and tooth surfaces in the oral cavity, and further, the function tends to be lowered after long-term storage.
[ Prior Art literature ]
[ Patent literature ]
Japanese patent application laid-open No. 10-511956
Japanese patent application laid-open No. 2009-137863 (patent document 2)
[ Patent document 3 ] International publication No. 2013/47826
Japanese patent application laid-open No. 2017-48162 (patent document 4)
Japanese patent application laid-open No. 2021-95380 (patent document 5)
Disclosure of Invention
[ Problem ] to be solved by the invention
The present invention has been made in view of the above circumstances, and an object thereof is to provide an oral composition which is excellent in fluoride ion retention on tooth surfaces and mucous membranes in the oral cavity and which can impart excellent fluoride ion retention even after long-term storage.
[ Means for solving the problems ]
The present inventors have intensively studied to achieve the above object and found that when (a) condensed phosphoric acid or a salt thereof, (B) a calcium salt, (C) a fluorine-containing compound and (D) pyrrolidone carboxylic acid or a salt thereof are combined and compounded in an oral composition, they are excellent in fluorine ion retention on tooth surfaces and mucous membranes in the oral cavity and can impart excellent fluorine ion retention even after long-term storage, and have completed the present invention.
If fluorine of the fluorine-containing compound blended in the oral composition is retained not only on the tooth surface but also on the oral mucosa sufficiently, it is expected that the retention in the oral cavity is further improved, but the oral mucosa is covered with salivary proteins such as mucin, and therefore fluorine is difficult to adsorb. In contrast, in the oral composition such as a dentifrice of the present invention, by combining the component (C) with the components (a) and (B), in addition to adsorption of fluoride ions to tooth surfaces (enamel), adsorption of fluoride ions to mucins covering the oral mucosa is also improved, so that the retention of fluoride ions is improved, and an effect of imparting a remarkably excellent retention is exhibited, whereby a relatively large amount of fluoride ions remain in the oral cavity after application. Further, by adding the component (D), the function can be prevented from decreasing even after long-term storage, and the effect of improving the retention of fluoride ions can be maintained, and in particular, the retention of fluoride ions to the oral mucosa can be made excellent.
The action and effect of the present invention can be obtained by combining the component (C) with the components (A), (B) and (D). As shown in the following comparative examples, the retention of fluoride ion on tooth surfaces and oral mucosa was poor (comparative examples 1 and 2) when the component (a) or (B) was not blended, and the retention of fluoride ion after long-term storage was also poor in comparative example 1 when the component (a) was not blended, and the retention of fluoride ion after long-term storage was poor (comparative example 3) when the component (D) was not blended. In contrast, in the oral composition containing components (a), (B), (C) and (D) according to the present invention, the retention of fluoride ions on the tooth surface and oral mucosa is excellent, and the retention of fluoride ions after long-term storage is excellent, as shown in examples.
In addition, in patent document 5 (japanese patent application laid-open No. 2021-95380), the retention and release of fluoride ions to the oral mucosa are improved by a combination of tripolyphosphate or pyrophosphate, a water-soluble calcium salt, sodium fluoride, and cationized cellulose. In contrast, the present invention can provide an excellent effect of retaining fluoride ions by improving the retention of fluoride ions on tooth surfaces and oral mucosa even after long-term storage by combining the components (a), (B), (C) and (D), particularly by specifically exerting unexpected actions on the component (D).
Accordingly, the present invention provides the following oral compositions.
[ 1] An oral composition comprising:
(A) Condensed phosphoric acid or its salt,
(B) Calcium salt,
(C) Fluorine-containing compound
And
(D) Pyrrolidone carboxylic acid or salts thereof.
〔2〕
The oral composition according to [1], wherein (A) the condensed phosphoric acid or a salt thereof is 1 or more selected from the group consisting of pyrophosphates, tripolyphosphates and metaphosphates.
〔3〕
The oral composition according to [ 2 ], wherein the condensed phosphoric acid or a salt thereof (A) is potassium pyrophosphate.
〔4〕
The oral composition according to any one of [1] to [ 3 ], wherein the calcium salt (B) is 1 or more selected from calcium chloride and calcium glycerophosphate.
〔5〕
The composition for oral cavity according to any one of [ 1 ] to [ 4 ], wherein the fluorine-containing compound (C) is 1 or more selected from sodium fluoride, sodium monofluorophosphate and tin fluoride.
〔6〕
The oral composition according to any one of [ 1] to [ 5 ], wherein (A)/(C) is 0.05 to 1 in a molar ratio and (B)/(C) is 0.1 to 2 in a molar ratio.
〔7〕
The oral composition according to any one of [1] to [ 6 ], wherein the content of the component (C) is 500 to 5,000ppm in terms of fluorine ion.
〔8〕
The composition for oral use according to any one of [1 ] to [ 7 ], wherein the content of the component (A) is 0.1 to 1.5% by mass, the content of the component (B) is 0.1 to 2% by mass, and the content of the component (D) is 0.1 to 10% by mass.
〔9〕
The oral composition according to any one of [1 ] to [ 8 ], wherein the oral composition is a dentifrice composition.
[ Effect of the invention ]
According to the present invention, there can be provided an oral composition containing a fluorine-containing compound which is excellent in the retention of fluorine ions on tooth surfaces and mucous membranes in the oral cavity and which can impart excellent retention of fluorine ions even after long-term storage. The oral composition of the present invention is excellent in the retention of fluoride ions on the tooth surface and also in the retention of fluoride ions on the oral mucosa, and therefore, by leaving a relatively large amount of fluoride ions in the oral cavity, it is possible to sufficiently exert the effects of the component (C) such as the promotion of recalcification and the inhibition of decalcification, and is effective for caries prevention.
Detailed Description
The present invention is described in further detail below.
The oral composition of the present invention comprises (A) a condensed phosphoric acid or a salt thereof, (B) a calcium salt, (C) a fluorine-containing compound, and (D) a pyrrolidone carboxylic acid or a salt thereof.
(A) The condensed phosphoric acid or a salt thereof exhibits an effect of improving the retention of fluorine ions, and also exhibits an effect of maintaining the effect of improving the retention of fluorine ions even after long-term storage.
As the condensed phosphoric acid or a salt thereof, a water-soluble condensed phosphoric acid or a salt thereof (solubility in water at 20 ℃ C. Is 1g/100g or more) can be preferably used. Examples thereof include linear polyphosphoric acid such as pyrophosphoric acid, tripolyphosphoric acid, and tetraphosphoric acid, and salts thereof, and cyclic polyphosphoric acid such as trimetaphosphoric acid, tetrametaphosphoric acid, and hexametaphosphoric acid, and salts thereof. Examples of the salt include alkali metal salts such as sodium salts and potassium salts. Among them, pyrophosphate, tripolyphosphate and metaphosphate are preferable, and pyrophosphate and tripolyphosphate are more preferable, in particular, from the viewpoint of improving the retention of fluoride ions after long-term storage.
Specific examples of the condensed phosphoric acid or a salt thereof include potassium pyrophosphate, sodium tripolyphosphate, sodium hexametaphosphate, and the like, and potassium pyrophosphate is particularly preferred.
These may be used singly or in combination of 1 or 2 or more, and commercially available products may be used.
(A) The amount of the condensed phosphoric acid or a salt thereof to be blended is preferably 0.1 to 1.5% by mass (the same applies hereinafter), more preferably 0.15 to 1.4%, and even more preferably 0.2 to 1.0% of the entire composition. When the blending amount is 0.1% or more, the retention of fluoride ions is sufficiently improved, the retention of fluoride ions on tooth surfaces and oral mucosa is excellent, and excellent retention of fluoride ions can be imparted even after long-term storage. When the concentration is 1.5% or less, the retention of fluorine ions can be sufficiently maintained.
(B) The calcium salt exerts an effect of improving the retention of fluoride ions.
The calcium salt is preferably a salt having a solubility in water of 0.5g/100g or more at 20 ℃. Examples thereof include calcium chloride, calcium glycerophosphate, calcium nitrate, calcium acetate, calcium citrate, calcium gluconate, calcium benzoate, calcium formate, calcium fumarate, calcium lactate, calcium butyrate, calcium isobutyrate, calcium malate, calcium maleate, calcium propionate, and calcium valerate. Among them, calcium chloride and calcium glycerophosphate are preferable, and calcium chloride is more preferable, in particular, from the viewpoint of improving the retention of fluoride ions after long-term storage.
These may be used singly or in combination of 1 or 2 or more, and commercially available products may be used.
(B) The amount of the calcium salt to be blended is preferably 0.1 to 2%, more preferably 0.1 to 1.5%, and still more preferably 0.2 to 1% of the entire composition. When the blending amount is 0.1% or more, the retention of fluoride ions is sufficiently improved, and the retention of fluoride ions on tooth surfaces and oral mucosa is excellent. When the concentration is 2% or less, the retention of fluorine ions can be sufficiently maintained.
As the fluorine-containing compound (C), fluorine-containing compounds such as sodium fluoride, sodium monofluorophosphate, and tin fluoride can be used. Among them, sodium fluoride is particularly preferred in view of the retention of fluoride ions after long-term storage.
These may be used singly or in combination of 1 or 2 or more, and commercially available products may be used.
The amount of the fluorine-containing compound (C) to be compounded is preferably 500 to 5,000ppm, more preferably 1,100 to 3,000ppm, based on fluorine ions, of the whole composition. When the amount of the fluorine ion is 500ppm or more, the retention of the fluorine ion can be sufficiently improved, and when the amount is 5,000ppm or less, the occurrence of a harmful effect such as plaque and teeth due to excessive intake can be prevented.
The amount of the fluorine-containing compound to be blended varies depending on the amount of the fluorine ions to be supplied, and for example, when sodium fluoride is used, the amount of the fluorine ions to be supplied is 0.11% of the total composition when 500ppm is used. Specifically, the compounding amount of sodium fluoride is preferably 0.11 to 1.1%, more preferably 0.25 to 0.7% of the entire composition.
In the present invention, the molar ratio of (A)/(C), which represents the ratio of the amount of the component (A) to the amount of the component (C), is preferably 0.05 to 1, more preferably 0.1 to 0.5.
The molar ratio of (B)/(C), which represents the ratio of the amounts of the component (B) and the component (C), is preferably 0.1 to 2, more preferably 0.2 to 1.
When the molar ratio of (A)/(C) and the molar ratio of (B)/(C) are each within the above-mentioned ranges, it is further preferable. When the component (C) is blended in such a molar ratio, the effect of improving the retention of fluorine ions on tooth surfaces and oral mucosa after long-term storage is more excellent.
(D) The pyrrolidone carboxylic acid or a salt thereof can maintain the effect of improving the retention of fluoride ions by the components (a) and (B) for a long period of time, and can exert the effect of improving the retention of fluoride ions even after long-term storage.
Examples of the pyrrolidone carboxylic acid or a salt thereof include alkali metal salts such as sodium salt and potassium salt of pyrrolidone carboxylic acid. Specifically, alkali metal salts of pyrrolidone carboxylic acid such as sodium pyrrolidone carboxylate can be used.
As the pyrrolidone carboxylic acid or its salt, commercially available ones can be used. For example, sodium pyrrolidone carboxylate may be used as the monosodium glutamate HEALTY SUPPLY CO., AJIDEW (registered trademark) N-50 manufactured by INC.
(D) The amount of pyrrolidone carboxylic acid or a salt thereof to be blended is preferably 0.1 to 10%, more preferably 0.5 to 5% of the entire composition. When the blending amount is 0.1% or more, the retention of fluorine ions can be sufficiently improved even after long-term storage. When the viscosity is 10% or less, a proper viscosity of the formulation can be sufficiently ensured. If the content is more than 10%, the viscosity of the formulation may increase, resulting in deterioration of extrudability.
The oral composition of the present invention can be formulated into a paste, gel, liquid, etc., in particular, into a dentifrice such as a toothpaste, gel dentifrice, liquid dentifrice, wet-powder dentifrice (tooth wet-powder dentifrice), mouthwash (mouthwash), oral spray, etc., and used. Particularly preferred are dentifrice compositions suitable as dentifrices such as toothpastes.
The preparation method can adopt conventional method according to the form and dosage form. The dentifrice composition can be formulated by a known method, and for example, can be obtained by compounding the components (a) to (D), water and any components by a conventional method.
In this case, any other component may be appropriately blended as required in addition to the above components according to the purpose, dosage form, and the like of the oral composition. Examples of the optional ingredients include surfactants, abrasives, thickeners, humectants, sweeteners, fragrances, preservatives, colorants, active ingredients, solvents, and the like.
Specific examples of any component are shown below. These optional ingredients may be blended singly or in combination of 1 or 2 or more, and the blending amount of each optional ingredient may be a conventional amount within a range not to hinder the effects of the present invention.
And (2) a surfactant:
examples of the surfactant include anionic surfactants, nonionic surfactants, and amphoteric surfactants, and the following (i) to (iii) are specific.
(I) Anionic surfactant
Examples thereof include alkyl sulfates such as dodecyl sulfate, acyl sarcosinates, acyl methyl taurates, acyl glutamates, and alpha-olefin sulfonates (tetradecene sulfonates). The above salts are preferably alkali metal salts such as sodium salts and potassium salts.
(Ii) Nonionic surfactant
Polyoxyethylene hydrogenated castor oil, polyoxyethylene alkyl ether, polyglycerin fatty acid ester, sorbitan fatty acid ester, and fatty acid monoglyceride are exemplified.
(Iii) Amphoteric surfactants
Examples thereof include fatty acid amidopropyl betaines such as coco fatty acid amidopropyl betaine and N-fatty acid acyl-N-carboxymethyl-N-hydroxyethyl ethylenediamine.
The amount of the surfactant to be blended is preferably 0.001 to 10%, particularly preferably 0.1 to 5% of the entire composition.
An abrasive:
Examples thereof include silica-based abrasives such as anhydrous silicic acid, zeolite, calcium carbonate, and aluminum hydroxide. The amount of the abrasive to be blended is usually 2 to 50%, particularly 10 to 40% of the entire composition.
And (3) a thickening agent:
Examples thereof include organic thickeners such as xanthan gum (Xanthan gum), sodium alginate, hydroxyethyl cellulose, carrageenan, sodium carboxymethyl cellulose, polyvinylpyrrolidone, sodium polyacrylate, cationized cellulose, and carboxyvinyl polymer, and inorganic thickeners such as thickening silica. The amount of thickener compounded is usually 0.1 to 10%, particularly 0.1 to 8% of the entire composition.
A wetting agent:
examples of the polyhydric alcohols include sugar alcohols such as sorbitol, xylitol and erythritol, and polyhydric alcohols such as glycerin, propylene glycol and polyethylene glycol (PEG). The amount of humectant blended is typically 2 to 50% of the composition as a whole.
Sweetener:
saccharin, sodium saccharin, and sucralose may be mentioned.
Perfume:
menthol, anethole, carvone, eugenol, limonene, n-decanol, citronellol, alpha-terpineol, citronellyl acetate, eucalyptol, linalool, ethyl linalool, vanillin, thymol, spearmint oil, peppermint oil, lemon oil, orange oil, sage oil, rosemary oil, cinnamon oil, multi-fragrant fruit oil, cassia oil, perilla oil, wintergreen oil, clove oil, eucalyptus oil, which may be used singly or in combination of1 or 2 or more. The amount of perfume compounded is usually 0.01 to 2% of the total composition.
Preservative:
parahydroxybenzoate and sodium benzoate are exemplified.
Coloring agent:
Examples of the pigment include blue No.1, blue No. 2, green No. 3, yellow No. 4, yellow No. 5, red No. 106, red No. 227, caramel, titanium oxide, and mica titanium.
Any effective components:
Examples of the enzyme include enzymes such as glucose dehydrogenase, allantoin, glycyrrhetate, glycyrrhetinic acid, sodium chloride, isopropyl methylphenol, copper gluconate, cetyl pyridinium chloride, benzalkonium chloride, benzethonium chloride, hinokitiol, zeolite, aluminum lactate, potassium nitrate, and phellodendron bark extract. The compounding amount of these effective ingredients may be an effective amount within a range that does not hinder the effects of the present invention.
Solvent:
examples thereof include purified water, ethanol, and other lower monohydric alcohols having 2 or 3 carbon atoms. In addition, when ethanol is blended, the content of ethanol may be 25% or less of the entire composition, or the ethanol may not be blended.
[ Example ]
The present invention will be specifically described with reference to the following examples and comparative examples, but the present invention is not limited to the following examples. In the following examples,% represents% by mass unless otherwise specified.
Examples and comparative examples
Dentifrice compositions (toothpastes) having the compositions shown in tables 1 to 4 were prepared by a conventional method and evaluated by the following methods. The results are also recorded in the table.
(1) Method for evaluating retention of fluorine ions on tooth surface
The dentifrice composition was diluted 4-fold with purified water, and the diluted solution was applied to a Hydroxyapatite (HA) disk (diameter: 7mm, thickness: 3.5mm, manufactured by PENTAX Co.) for 3 minutes, and immediately washed with purified water. After drying the HA disk, the upper surface of the HA disk was decalcified with 120. Mu.L of 0.1N HCl for 2 minutes, and fluorine ions were extracted, and the fluorine ions contained in the solution were measured by an ion meter (Orion 1115000 4-Star, manufactured by Thermo FISHER SCIENTIFIC Co.) to determine the fluorine ion concentration (ppm), and the evaluation was performed based on the following criteria.
Evaluation criterion for the retention of fluoride ions on tooth surfaces
And (3) the following materials: the concentration of fluoride ion is above 2.0ppm
And (2) the following steps: the concentration of fluorine ions is more than 1.5ppm and less than 2.0ppm
Delta: the concentration of fluorine ions is more than 1.0ppm and less than 1.5ppm
X: fluoride ion concentration of less than 1.0ppm
(2) Method for evaluating retention of fluoride ion on oral mucosa
To a 10mL centrifuge tube, 0.2g of mucin (manufactured by Sigma-Aldrich) was added, and a further 10mL of the dentifrice composition (4-fold dilution with purified water) was added to allow to act for 3 minutes. Then, the mixture was centrifuged at 10,000rpm for 10 minutes, and the supernatant was removed. To mucin, 10mL of potassium citrate buffer was added, and the mixture was stirred for 1 minute to dissolve out fluorine ions adsorbed/retained on mucin. The supernatant was collected by centrifugation at 10,000rpm for 10 minutes, and the concentration of fluorine ions (ppm) contained in the solution was measured by a fluorimeter (Orion 11150004-Star, manufactured by Thermo FISHER SCIENTIFIC Co.) to evaluate the retention of fluorine ions in the oral mucosa based on the following criteria.
Evaluation criterion for the retention of fluoride ions in oral mucosa
And (3) the following materials: the concentration of fluoride ion is above 100ppm
And (2) the following steps: the concentration of fluorine ions is more than 60ppm and less than 100ppm
Delta: the concentration of fluorine ions is more than 30ppm and less than 60ppm
X: fluoride ion concentration of less than 30ppm
(3) Method for evaluating retention of fluorine ions after long-term storage
To 3 test tube containers (raw material: an innermost layer was a 26mm diameter laminated tube composed of linear low density polyethylene, manufactured by Daiko printing Co., ltd.) were added 50g of the dentifrice composition, and the mixture was stored at 40℃for 1 month. The fluoride ion retention of the dentifrice composition recovered to normal temperature after storage was evaluated by the same method as in (2) above, and the fluoride ion concentration (retained fluoride ion concentration (ppm)) of the long-term stored product was measured and determined.
The fluorine ion retention (%) of the non-preserved dentifrice composition obtained by the method (2) was calculated by the following formula, assuming that the fluorine ion concentration of the non-preserved dentifrice composition was the retained fluorine ion concentration (ppm) of the initial product, and the fluorine ion retention after long-term preservation was evaluated based on the following criteria.
Fluorine ion retention (%) =
Evaluation criterion of the fluorine ion retention after { (retained fluorine ion concentration (ppm) of Long-term storage article)/(retained fluorine ion concentration (ppm) of initial article) } ×100 long-term storage
And (3) the following materials: the retention rate of fluorine ions is more than 80 percent
And (2) the following steps: the retention rate of fluorine ions is more than 50% and less than 80%
Delta: the retention rate of fluorine ions is more than 20% and less than 50%
X: the retention rate of fluorine ions is less than 20 percent
The detailed information of the raw materials used is as follows.
(A) Potassium pyrophosphate: manufactured by Taiping chemical industry Co Ltd
(A) Sodium pyrophosphate: sodium pyrophosphate (anhydrous) manufactured by Taiping chemical industry Co., ltd
(A) Sodium tripolyphosphate: manufactured by Taiping chemical industry Co Ltd
(B) Calcium chloride: manufactured by Kanto chemical Co., ltd
(B) Calcium glycerophosphate: manufactured by Shicheng fruit Co Ltd
(C) Sodium fluoride: styrax chemical (STELLA CHEMIFA) Co., ltd
(D) Sodium pyrrolidone carboxylate: weisu HEALTY SUPPLY CO., INC, AJIDEW (registered trademark) N-50
[ Table 1]
[ Table 2]
[ Table 3]
[ Table 4]

Claims (9)

1. An oral composition comprising (A) a condensed phosphoric acid or a salt thereof,
(B) Calcium salt,
(C) Fluorine-containing compound
And
(D) Pyrrolidone carboxylic acid or salts thereof.
2. The oral composition according to claim 1, wherein (a) the condensed phosphoric acid or a salt thereof is 1 or more selected from the group consisting of pyrophosphates, tripolyphosphates and metaphosphates.
3. The oral composition of claim 2, wherein (a) the condensed phosphoric acid or salt thereof is potassium pyrophosphate.
4. The oral composition according to claim 1, wherein (B) the calcium salt is 1 or more selected from the group consisting of calcium chloride and calcium glycerophosphate.
5. The oral composition according to claim 1, wherein the fluorine-containing compound (C) is 1 or more selected from the group consisting of sodium fluoride, sodium monofluorophosphate and tin fluoride.
6. The oral composition according to claim 1, wherein (a)/(C) is 0.05 to 1 in molar ratio and (B)/(C) is 0.1 to 2 in molar ratio.
7. The oral composition according to claim 1, wherein the content of the component (C) is 500 to 5,000ppm in terms of fluorine ion.
8. The composition for oral use according to claim 1, wherein the content of the component (A) is 0.1 to 1.5% by mass, the content of the component (B) is 0.1 to 2% by mass, and the content of the component (D) is 0.1 to 10% by mass.
9. The oral composition of any one of claims 1-8, wherein the oral composition is a dentifrice composition.
CN202280063104.XA 2021-10-12 2022-10-05 Oral composition Pending CN118076334A (en)

Applications Claiming Priority (3)

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JP2021-167095 2021-10-12
JP2021167095 2021-10-12
PCT/JP2022/037212 WO2023063180A1 (en) 2021-10-12 2022-10-05 Oral composition

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